吡罗昔康Β环糊精 | 96684-40-1

• 物质功能分类: 原料药 - 解热镇痛药 - 非甾抗炎药
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 吡罗昔康Β环糊精
• 中文别名: 吡罗昔康倍他环糊精
• 英文名称: 1:2.5 piroxicam-β-cyclodextrin complex
• 英文别名: Piroxicam-beta-cyclodextrin；(1S,3R,5R,6S,8R,10R,11S,13R,15R,16S,18R,20R,21S,23R,25R,26S,28R,30R,31S,33R,35R,36R,37R,38R,39R,40R,41R,42R,43R,44R,45R,46R,47R,48R,49R)-5,10,15,20,25,30,35-heptakis(hydroxymethyl)-2,4,7,9,12,14,17,19,22,24,27,29,32,34-tetradecaoxaoctacyclo[31.2.2.23,6.28,11.213,16.218,21.223,26.228,31]nonatetracontane-36,37,38,39,40,41,42,43,44,45,46,47,48,49-tetradecol;4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-yl-1λ6,2-benzothiazine-3-carboxamide
• CAS: 96684-40-1；96684-39-8
• 化学式: C₁₅H₁₃N₃O₄S*2C₄₂H₇₀O₃₅
• 分子量: 3168.84
• InChiKey: LBPBSKKEZXLVBQ-ZQOBQRRWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -13.65
• 重原子数：
  100
• 可旋转键数：
  9
• 环数：
  24.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  662
• 氢给体数：
  23
• 氢受体数：
  41

制备方法与用途

简介

吡罗昔康倍他环糊精（又称炎痛昔康倍他环糊精）是采用独特工艺路线，按一定比例将医药级的吡罗昔康与医药级的倍他环糊精包合精制而成。吡罗昔康属于非甾体抗炎药的一种，其抗炎作用强，但难溶于水、吸收缓慢，口服后易导致胃肠道出血和胃溃疡，肌注给药可能引起注射部位疼痛和轻度组织坏死。将吡罗昔康制备成吡罗昔康-β-环糊精（piroxicam-β-cyclodextrin）包合物后，可以加快药物的溶出速度，降低对胃肠道的刺激性。口服镇痛药喜来通（cycladol）即为吡罗昔康-β-环糊精包合物的成功应用。

应用

吡罗昔康倍他环糊精（又称炎痛昔康倍他环糊精）是通过独特工艺路线，按一定比例将医药级的吡罗昔康与医药级的倍他环糊精包合精制而成。该包合物相较于吡罗昔康单体具有更低的气味、更强的稳定性以及更平稳的药物释放速度等优点，并主要应用于消炎镇痛药剂和制药辅料。

反应信息

• 作为产物：
  描述：

  吡罗昔康 、 β-环糊精 在 氨 作用下， 以 水 为溶剂， 反应 0.5h， 生成 吡罗昔康Β环糊精
  参考文献：
  名称：

  [EN] A PROCESS FOR THE PREPARATION OF A PIROXICAM: BETA­CYCLODEXTRIN INCLUSION COMPOUND
  [FR] PROCEDE POUR LA PREPARATION D'UN PIROXICAME: COMPOSE D'INCLUSION A BASE DE BETA-CYCLODEXTRINE

  摘要：

  公开号：

  WO2006013039A3

文献信息

• PIPERIDIN-2-ONE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1447401A1

  公开（公告）日：2004-08-18

  A piperidin-2-one derivative compound represented by formula (I): wherein all symbols are described in the specification, or a non-toxic salt thereof. The compound represented by formula (I) inhibits activation of p38MAP kinase, and is useful for prevention and/or treatment of various inflammatory diseases, rheumatoid arthritis, osteoarthritis, arthritis, osteoporosis, autoimmune diseases, infectious diseases, sepsis, cachexia, cerebral infarction, Alzheimer's disease, asthma, chronic pulmonary inflammatory diseases, reperfusion injury, thrombosis, glomerulonephritis, diabetes, graft versus host rejection, inflammatory bowel disease, Crohn's disease, ulcerative colitis, multiple sclerosis, tumor growth and metastasis, multiple myeloma, plasma cell leukemia, Castleman's disease, atrial myxoma, psoriasis, dermatitis, gout, adult respiratory distress syndrome (ARDS), arteriosclerosis, post-percutaneous transluminal coronary angioplasty (PTCA) restenosis or pancreatitis.

  一个由公式(I)表示的哌啶-2-酮衍生物化合物： 其中所有符号都在说明书中描述，或其无毒盐。 由公式(I)表示的化合物能抑制p38MAP激酶的激活，并且可用于预防或治疗各种炎症性疾病、类风湿性关节炎、骨关节炎、关节炎、骨质疏松症、自身免疫病、感染性疾病、败血症、恶病质、脑梗塞、阿尔茨海默病、哮喘、慢性肺泡炎、再灌注损伤、血栓形成、肾小球肾炎、糖尿病、移植物抗宿主病、炎症性肠病、克罗恩病、溃疡性结肠炎、多发性硬化症、肿瘤生长和转移、多发性骨髓瘤、浆细胞白血病、卡斯尔曼病、心房粘液瘤、银屑病、皮炎、痛风、成人呼吸窘迫综合征（ARDS）、动脉硬化、经皮腔内冠状动脉成形术（PTCA）后再狭窄或胰腺炎。
• NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND MEDICINAL USE THEREOF
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1741702A1

  公开（公告）日：2007-01-10

  The present invention provides a compound having p38 MAP kinase inhibitory activity. Because of having p38 MAP kinase inhibitory activity, the compounds represented by the formula (I): wherein each symbol is as defined in the description, salts thereof, N-oxides thereof, solvates thereof, or prodrugs thereof are useful in preventing and/or treating diseases that are supposedly caused or deteriorated by abnormal production of cytokines including inflammatory cytokines or chemokines, or by overresponse thereto, namely cytokine-mediated diseases such as inflammatory diseases, respiratory diseases, cardiovascular diseases and bone diseases.

  本发明提供了一种具有p38 MAP激酶抑制活性的化合物。由于具有p38 MAP激酶抑制活性，由式(I)所表示的化合物：其中每个符号如描述中所定义，其盐、N-氧化物、溶剂合物或前药在预防和/或治疗据称由细胞因子异常产生或恶化引起的疾病方面具有用处，包括炎症性细胞因子或趋化因子，或由对其过度反应引起的疾病，即细胞因子介导的疾病，如炎症性疾病、呼吸系统疾病、心血管疾病和骨疾病。
• REMEDY FOR CHRONIC DISEASE
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1550461A1

  公开（公告）日：2005-07-06

  A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the progress of chronic asthma, glomerular nephritis, obesity, arteriosclerosis, rheumatoid and atopic diseases) induced and made chronic by tissue cells whose proliferation is accelerated by LPA mediated by EDG-2.

  一种包含EDG-2拮抗剂的慢性疾病的治疗和/或预防药物。由于结合到LPA受体的亚型EDG-2，EDG-2拮抗剂在治疗和/或预防慢性疾病方面是有用的（例如，由EDG-2介导的LPA加速组织细胞增殖导致并使之慢性化的慢性哮喘、肾小球肾炎、肥胖、动脉硬化、风湿和特应性疾病等疾病）。
• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。
• [EN] PYRROLOTRIAZINE COMPOUNDS<br/>[FR] COMPOSÉS DE PYRROLOTRIAZINE
  申请人：LOCUS PHARMACEUTICALS INC

  公开号：WO2010126960A1

  公开（公告）日：2010-11-04

  A compound of formula (I), wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.

  具有式（I）的化合物，其中所有符号的含义与规范中定义的相同；其盐、溶剂合物、N-氧化物或前药具有Btk抑制活性，并且可用作预防和/或治疗类风湿关节炎、自身免疫疾病、B细胞淋巴瘤或癌症等的方法。